Clopidogrel

Name: Clopidogrel (Plavix)

Mode of action:

Clopidogrel - antiplatelet drug. Effect of the drug is carried through the ability of clopidogrel selectively inhibit the binding of adenosine diphosphate receptors of platelets, thus inhibited the activation of a complex glycoprotein IIb / IIIa and decreases the ability of platelets to aggregate. The drug increases the bleeding time. Antiplatelet effect of clopidogrel is dose-dependent, when using the drug at the recommended therapeutic doses, the maximum therapeutic effect occurs within 3-7 days. The drug irreversibly blocks the platelet ADP receptor, so that they lose the ability to aggregate, the restoration of normal function of the observed 7 days after drug withdrawal, as the renovation of platelets.

After oral administration of the drug is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 50% and is independent of food intake. Clopidogrel - a prodrug, is metabolized in the liver to the active substance - thiol metabolite of clopidogrel. The main metabolite is the carboxylic derivative, which is determined by the pharmacokinetic profile. The peak drug concentration in plasma was after 60 minutes after oral administration. Excreted in the urine and feces as metabolites. The half-life is approximately 8 hours.

Indications for use:

The drug is used as a prophylactic agent in patients suffering from cardio-vascular system, in particular for the prevention of atherothrombotic events in patients with myocardial infarction, ischemic stroke, and patients with peripheral arterial disease. The drug is also used in combination with acetylsalicylic acid for the treatment of acute coronary syndrome without elevation ST (in particular, patients with unstable angina or myocardial infarction without tooth Q).
Clopidogrel is used in treatment of patients with acute myocardial infarction with elevation ST, in the case where a patient for thrombolytic therapy.

Method of application:

The drug is taken orally. The tablet is recommended to swallow whole without chewing or crushing, drinking plenty of water. Acceptance of the drug is independent of food intake. The duration of treatment and dose is usually determined by the attending physician for each patient individually.
Adults and elderly patients for the prevention of atherothrombotic events is usually prescribed for drug 75mg (1 tablet) 1 every day. Receiving the drug for the prevention of post-myocardial infarction should be started within a few days, but no later than 35 days later, after ischemic stroke - after a week, but no later than 6 months. Patients with acute coronary syndromes without ST-segment elevation is usually administered once 300mg of the drug (4 tablets) at baseline, and then move on to receive 75 mg of the drug 1 per day in combination with acetylsalicylic acid. Dose of acetylsalicylic acid determined by the attending physician individually, usually it is 75-325mg per day, however, due to the increased risk of bleeding not exceed the recommended daily dose of aspirin 100 mg. The maximum therapeutic effect is observed at 3 months after initiation of therapy.

In acute myocardial infarction is usually administered once 300mg of the drug at the beginning of treatment, and then move on to the application of 75 mg of the drug 1 per day in combination with acetylsalicylic acid. For patients older than 75 years of the drug begin with 75 mg of the drug one time per day, skipping a loading dose of the drug at the beginning of therapy. Duration of treatment for at least 4 weeks.
Data on the need for dose adjustment of the drug in patients with impaired liver function and / or kidney disease are lacking.

Side effects of Clopidogrel:

Using the drug Clopidogrel in patients noted the development of adverse reactions:
Blood system: thrombocytopenia, granulocytopenia, neutropenia, anemia (including aplastic anemia), and in rare cases noted the development of thrombotic thrombocytopenic purpura syndrome (Moshkovitsa) and purpura Henoch-Schonlein. It is also often noted the development of different localization of bleeding in patients receiving the drug clopidogrel, including gastrointestinal and nasal bleeding, as well as ocular and intracranial hemorrhage

Gastro-intestinal tract and liver: stomatitis, nausea, vomiting, dyspepsia, epigastric pain, stool disorders, gastritis and peptic ulcer and duodenal ulcer. In addition, the possible increase in liver enzymes and increased levels of bilirubin in the blood.

Allergic reactions: skin rash, itching, rash, maculopapular rash, bronchospasm, angioedema.

Other: cough, arrhythmia, pulmonary embolism, fatigue, confusion, headache, fever, myalgia, arthralgia, hematuria.
With the development of side effects, stop taking the medication and call your doctor.
In case of bleeding, including hidden, you should contact your doctor as the drug prolong bleeding time and increases the risk of bleeding complications. If excessive bleeding is noted the development, including bleeding gums, it is necessary to conduct a study of the hemostatic system, in addition, when using the drug clopidogrel is recommended to regularly monitor liver function.
Patients taking clopidogrel should inform health professionals (including dentists) of this medication.

Contraindications:

Increased individual sensitivity to the drug.
Severe liver problems, jaundice, accompanied by cholestasis. Due to the fact that the product contains lactose, it is not indicated for patients with malabsorption of glucose-galactose lactase deficiency and hereditary.
The drug is not used for the treatment of patients with active bleeding, including bleeding from peptic peptide or intracranial hemorrhage.
The drug is contraindicated during pregnancy and breastfeeding.

In view of the unproven efficacy and safety of the drug in patients under 18 years of clopidogrel should not be used in pediatrics. The drug should be used with caution in patients with an increased risk of bleeding due to trauma, surgical interventions, as well as violations of the blood system.
The drug should be used with caution in patients suffering from impaired renal function and / or liver.
Do not take the drug for 7 days before elective surgery.

Pregnancy:

The drug is contraindicated in pregnancy due to the fact that the safety of the drug to the fetus has not been proved. If necessary, use during lactation should decide the issue of a possible interruption of breastfeeding.

Interactions with other drugs:

If concomitant use of medication with acetylsalicylic acid indicated mutual enhancement of their effect on platelet aggregation. Safety of combined treatment with these drugs for more than 12 months has not been proved.
The drug should be used cautiously in conjunction with heparin, but the use of the drug clopidogrel in patients receiving heparin therapy does not require dose adjustment of the latter.
When a drug to patients taking other thrombolytic drugs, caution should be exercised.
With the simultaneous use of clopidogrel with warfarin may increase the risk of bleeding. You should not assign clopidogrel in patients receiving warfarin therapy.

The drug should be used with caution with drugs that have a high degree of correlation with plasma proteins.
When concomitant administration of drugs with non-steroidal anti-inflammatory drugs with caution.
With the simultaneous use of the drug with antacids drugs were no changes in pharmacokinetic parameters of clopidogrel.
Caution must be exercised in the appointment of Clopidogrel in patients receiving inhibitors of glycoprotein IIb / IIIa.

Overdose:

In the application of excessive doses of the drug in patients observed an increase in bleeding time.
No specific antidote. In case of overdose symptomatic treatment is shown. In the case require immediate correction of the state, shows a transfusion of platelets.

Product:

Film-coated tablets, 10 pieces per blister, 1 or 2 blisters in a carton.